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7612067 |
Imidazopyridazine compounds
The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I): pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing...
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7601719 |
Compounds, methods and pharmaceutical compositions for inhibiting PARP
The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat,...
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7598247 |
Immunomodulating heterocyclic compounds
Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy:
wherein R 1 and R 3 independently represent H; F; Cl; Br; —NO 2 ; —CN; C 1 -C 6 alkyl optionally...
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7595324 |
Substituted thieno[3,2-D]pyrimidines as HIV inhibitors
This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I
where the dashed line represents a double bond that may be located either between A and C(V)...
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7589105 |
Preventives or remedies for alzheimer's disease, or amyloid protein fibril-formation inhibitors, which include a nitrogen-containing heteroaryl compound
Pharmaceutical compositions and methods of treatment are provided for treating amyloidosis, containing, as an active ingredient, at least one nitrogen-containing heteroaryl compound represented by...
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7585873 |
1-(aminoalkyl)-3-sulfonylazaindoles as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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7582631 |
Substituted heterocyclic compounds and methods of use
The present invention relates to therapeutic diazobicyclo pyridines and their use in the treatment of arthritis, rheumatoid arthritis, psoriatic arthritis or osteoarthritis, organ transplant, acute...
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7582630 |
Pyradazine compounds as GSK-3 inhibitors
The present invention relates to pyrazaolpyradazine derivatives that inhibit GSK3 (glycogen synthase kinase), pharmaceutical compositions containing these derivatives, and methods for their use in...
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7579348 |
Derivatives of 8-substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I
which are selective antagonists of A 2B adenosine receptors...
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7569574 |
Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
The invention relates to new purine derivatives of general formula
wherein R 1 to R 4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and...
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7569567 |
3-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use
A subject-matter of the invention is the compounds of general formula (I)
in which X represents a hydrogen or halogen atom;
R 1 represents a hydrogen atom or a (C 1 -C 4 )alkyl group; R 2 ...
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7566713 |
Immuno inhibitory heterocyclic compounds
Compounds of formula (I) are CD80 inhibitors, and of value for immunomodulation, e.g. in rheumatoid arthritis, multiple sclerosis, diabetes, asthma, transplantation, systemic lupus erythematosis...
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7566707 |
Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula
wherein Y and R 1 to R 4 are defined as in claim 1 , the tautomers, enantiomers,...
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7563790 |
Pyridazine derivatives
Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis,...
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7563773 |
Anthelmintic oral homogeneous veterinary pastes
This invention provides for, inter alia, oral homogeneous veterinary pastes for the treating, controlling and preventing of endo- and ectoparasite infections in warm-blooded animals or birds, such...
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7560551 |
Aurora kinase modulators and method of use
The present invention relates to chemical compounds having a general formula I
wherein A 1 , A 2 , C 1 , C 2 , D, L 1 , L 2 , Z and R 1-8 are defined herein, and synthetic intermediates, which...
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7557103 |
Imidazopyridazine compounds
The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I) pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing...
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7550461 |
Benzofuran and benzothiophene compounds useful in treating cytokine mediated diseases
Disclosed are amide compounds of formula (I):
wherein Ar 1 , Q, Y and R 3 -R 6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory...
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RE40793 |
Bicyclic benzamides of 3-or 4-substituted 4-(aminomethyl)-piperidine derivatives
The present invention of compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 and R 2 ...
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7547698 |
Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coadesaturase (SCD)
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a...
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7547697 |
Alkyl-pyridazine derivatives as 11b-HSD1 inhibitors
Compounds of formula (I):
as well as pharmaceutically acceptable salts and esters thereof for use as pharmaceutical compositions.
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7544684 |
Hydrazono-malonitriles
Hydrazono-malonitrile derivatives of the formula (I) in which R 1 , R 2 , R 3 , R 3′ and R 4 have the meanings given in Claim 1 act as phosphodiesterase IV inhibitors and can be employed for...
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7541364 |
Pyridomorphinans, pyridazinomorphinans and use thereof
Compounds represented by the formula:
wherein R is C 1-6 alkyl; C 4-6 cycloalkylalkyl; or C 3-6 alkenyl; R′ is H or C 1-6 alkyl; X is H or OH; Y is alkyl, cycloalkyl, aryl, heteroaryl,...
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7534795 |
Compounds and their use related to compositions for treating disease
Novel compounds and their uses are disclosed herein.
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7534793 |
Aminopiperidine quinolines and their azaisosteric analogues with antibacterial activity
Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man
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7531540 |
Phthalazinone-piperidino-derivatives as PDE4 inhibitors
The compounds of formula I
in which the given substituents have the meanings as given in the description, are novel effective PDE4 inhibitors.
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7528139 |
Sulfonamides
Compounds of the formula (I), in which R 6 , R 7 , R 8 , R 9 and X have the meanings indicated in claim 1 , are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be...
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7524845 |
Azaindazole compounds and methods of use
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in...
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7517883 |
Solubilized topoisomerase poisons
The invention provides compounds of formula I:
wherein
A, B, W, Y, Z, and R 1 have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention...
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7511039 |
β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are...
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7501410 |
Methods of inhibiting BTK and SYK protein kinases
Methods of inhibiting a tyrosine kinase wherein said tyrosine kinase is BTK or SYK comprising administering to a patient in need thereof a therapeutically effective amount of a compound according...
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7488739 |
Quinolone derivative or salt thereof
A platelet aggregation inhibitor comprising a quinolone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a novel quinolone derivative or a pharmaceutically...
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7485641 |
Substituted 3-amino-pyrrolidino-4-lactams
The invention provides compounds of formula (1),
and the pharmaceutically acceptable salt thereof, wherein R 1 , n and R 2 are as described herein; compositions thereof; and uses thereof.
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7482345 |
P38 kinase inhibiting agents
Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof:
are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of...
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7476763 |
Oxo-substituted cyclohexyl-1,4-diamine compounds
Novel cyclohexyl-1,4-diamine compounds corresponding to formula I:
methods for their production, pharmaceutical formulations containing these compounds, methods of producing such pharmaceutical...
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7459564 |
Substituted biaryl compounds as factor XIa inhibitors
The present invention provides compounds of Formula (I):
or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R 3 , and ring B...
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7459454 |
Aminopyrazine derivatives and compositions
The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and...
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7456195 |
Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV):
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein...
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7456177 |
Heteroaryl fused azapolycyclic compounds
The present invention provides a compound having the structure of formula I:
wherein R 1 is hydrogen, (C 1 –C 6 ) alkyl, unconjugated (C 3 –C 6 ) alkenyl, benzyl, YC(═O)(C 1 –C 6 )...
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7452880 |
Substituted pyrazolo [3,4-d] pyrimidines and methods of using the same
Compounds of the formula I:
where A, B, X, Y, Z, k, R 1 , R 2 and R 3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing...
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7449464 |
Phthalazinone derivatives
Compounds of the formula (I):
wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NR X or CR X R Y ; if X=NR X then n is 1 or 2 and if X=CR X R Y then...
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7446113 |
Acetylenyl-pyrazolo-pyrimidine derivatives
The present invention relates to compounds of formula (I):
wherein R 1 to R 3 , A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for...
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7442699 |
Anilinopyrimidine derivatives as IKK inhibitors and compositions and methods related thereto
Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure:
wherein R 1 ...
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7432262 |
Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions
The invention relates to substituted imidazopyridazinediones of general formula
wherein R 1 to R 4 are defined as in claim 1 , the tautomers, the enantiomers, the diastereomers, the mixtures...
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7429581 |
Pyrazole-derivatives as factor Xa inhibitors
The present invention is directed to a compound of formula I,
in which R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; Q; V, G and M have the meanings indicated below. The compound of formula I is a...
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7423030 |
1-amino-phthalazine derivatives, the preparation and the therapeutic use thereof
A 1-amino-phthalazine derivative of general formula (I)
wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such...
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7417062 |
Substituted arylamides
Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.
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7417041 |
Imidazopyrimidines as transforming growth factor (TGF) inhibitors
Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described....
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7407964 |
Caspase inhibitors and uses thereof
This invention provides novel caspase inhibitors of formula I:
wherein R 1 is hydrogen, CHN 2 , R, or —CH 2 Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group,...
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7407950 |
N-(heteroaryl)-1H-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands
The invention concerns compounds of general formula (I), wherein n, X 1 , X 2 , X 3 , X 4 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 and W are as defined herein.
Said compounds are ligands of the TRPV 1 ...
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